Pipeline

Rigorous and groundbreaking science has always been at the core of what we do at Genentech. Our R&D activities are focused on applying excellent science to discover and develop potential new medicines with the goal of becoming first-in-class or best-in-class therapeutics.

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MOLECULES

Oncology

Immunology

Neuroscience

Metabolism

Infectious Disease

Ophthalmology

Phase IPhase IIPhase III

Managed by Roche

Molecule

Indication

Phase

Alectinib

ALK+ metastatic non-small cell lung cancer

Alectinib is a small molecule designed to selectively target ALK (anaplastic lymphoma kinase).

Mechanism of Action / Target

Alectinib is designed to bind to ALK and block downstream signaling pathways, such as STAT3, PIK3/AKT and MAPK

Anti-OX40 (MOXR0916, RG7888), a humanized monoclonal antibody, is designed to target OX40, a costimulatory receptor that is selectively expressed on the surface of antigen-experienced T cells. Anti-OX40 functions as an agonist antibody, which results in activation rather than blockade, of the OX40 signaling pathway upon receptor binding.

Anti-STEAP1 (DSTP3086S, RG7450) is an antibody drug conjugate (ADC) that consists of a humanized monoclonal antibody directed against STEAP1, a six-transmembrane epithelial antigen of the prostate 1, conjugated to an anti-mitotic agent, monomethyl auristatin E (MMAE). STEAP1 is a membrane protein that is overexpressed in prostate cancer.

GDC-0199 (RG7601) is a small molecule Bcl-2 selective inhibitor designed to restore apoptosis, also known as programmed cell death, by blocking the function of a pro-survival Bcl-2 family protein. The Bcl-2 family proteins, which are expressed at high levels in many tumors, play a central role in regulating apoptosis.

Mechanism of Action / Target

Apoptosis, Bcl-2 selective inhibitor

Status

A Phase I trial evaluating GDC-0199 for chronic lymphocytic leukemia and non-Hodgkin's lymphoma is ongoing, and a Phase I trial evaluating GDC-0199 in combination with Rituxan® (Rituximab) for non-Hodgkin's lymphoma is planned.

Bevacizumab (Avastin) is a monoclonal antibody that is designed to specifically bind and block the biological effects of VEGF (vascular endothelial growth factor) protein on blood vessel cells. The tumor blood supply is thought to be critical to a tumor’s ability to grow and spread in the body (metastasize) to other parts of the body. It is being investigated in a variety of solid cancers.

GDC-0575 (RG7741) is a small molecule ChK1 selective inhibitor designed to prevent tumor cells from recovering from DNA damage.

Checkpoint kinase 1 (ChK1) is a protein kinase that regulates tumor cells' response to DNA damage. In response to DNA damage, ChK1 blocks cell cycle progression in order to allow for repair of damaged DNA. This is being tested for its effect on tumor cell death.

Mechanism of Action / Target

Cell cycle signaling, checkpoint kinase 1 (ChK1) inhibitor

This molecule is being developed by Genentech as part of an oncology agreement with Array BioPharma.

GDC-0973 (RG7421), a selective inhibitor of MEK, also known as mitogen activated protein kinase kinase (MAPKK), is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors. Inappropriate activation of the MEK/ERK pathway promotes cell growth in the absence of exogenous growth factors.

Mechanism of Action / Target

Status

A Phase III and a Phase Ib clinical trial in combination with Zelboraf® (vemurafenib) for metastatic melanoma; a Phase Ib clinical trial in combination with GDC-0068, an Akt Inhibitor, for solid tumors; and a Phase Ib clinical trial in combination with GDC-0941, a PI3 Kinase Inhibitor, for solid tumors are ongoing. A Phase I clinical trial evaluating GDC-0973 as a single agent in solid tumor is ongoing.GDC-0973 is being developed in collaboration with Exelixis, Inc. and Zelboraf is being developed in collaboration with Plexxikon, Inc. co-developed under a 2006 license and collaboration agreement between Roche/Genentech and Plexxikon, a member of the Daiichi Sankyo Group.For Zelboraf full prescribing information, including Medication Guide and important safety information, please visit http://www.zelboraf.com.

GDC-0994 (RG7842) is a selective inhibitor of ERK1/2, also known as extracellular-signal-regulated kinases. ERK is a key component of the RAS/RAF/MEK/ERK signaling pathway, which is frequently activated in human tumors. Inappropriate activation of the MEK/ERK pathway promotes cell growth in the absence of exogenous growth factors.

GDC-0919 (NLG919, RG6078) is a small molecule investigational immunotherapy designed to inhibit IDO (Indoleamine 2,3-dioxygenase), a protein often overproduced by many cancer cells. This molecule is being developed in collaboration with NewLink Genetics Corporation.

Onartuzumab, MetMAb, is a monoclonal monovalent (one-armed) antibody designed to inhibit Met signalling in cancer cells by binding to the extracellular domain of Met, thereby blocking HGF-mediated activation. HGF/Met signalling is activated through over expression of either HGF and/or Met in tumours as well as through activating mutations in Met.

Pertuzumab (Perjeta) is a humanized monoclonal antibody designed to prevent HER2 dimerisation, a process that is believed to play an important role in the growth and formation of several different cancer types.

For Perjeta full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.perjeta.com or call:1-888-249-4918.

Pictilisib (GDC-0941, RG7321) is a small molecule specific Class I PI3 kinase inhibitor. PI3 Kinase is an oncogene that is commonly mutated in cancer. The PI3K/Akt/mTOR pathway regulates cell growth and survival.

Polatuzumab vedotin (Anti-CD79b, DCDS4501A, RG7596) is an antibody drug conjugate (ADC) composed of a monoclonal antibody directed against CD79b, link to the small molecule, cytotoxic, microtubule-disrupting agent, monomethyl auristatin E (MMAE). Polatuzumab vedotin is designed to selectively bind to CD79b on hematologic cells.

Mechanism of Action / Target

Antibody drug conjugate; anti-CD79b

Status

A Phase II clinical trial evaluating either pinatuzumab vedotin or polatuzumab vedotin in combination with Rituxan® (Rituximab) for relapsed or refractory follicular non-Hodgkin's lymphoma and relapsed or refractory diffuse large B-cell lymphoma is ongoing.

This molecule is being developed utilizing Seattle Genetics' ADC technology.

GDC-0810 (ARN-810, RG6046) is a selective estrogen receptor degrader (SERD) that is designed to bind to the estrogen receptor to limit its function. In addition, when SERDs bind to the estrogen receptor, they may be able to change the shape of the receptor in such a way that the cell eliminates it by degradation.

Mechanism of Action / Target

GDC-0927 (SRN-927, RG6047) is a selective estrogen receptor degrader (SERD) that is designed to bind to the estrogen receptor to limit its function. In addition, when SERDs bind to the estrogen receptor, they may be able to change the shape of the receptor in such a way that the cell eliminates it by degradation.

Vemurafenib (Zelboraf) is an oral, small molecule, BRAF kinase inhibitor. The BRAF protein is a key component of the RAS-RAF pathway involved in normal cell growth and survival. Mutations that keep the BRAF protein in an active state may cause excessive pathway signalling, leading to uncontrolled cell growth and survival.

Etrolizumab (rhuMAb Beta7, RG7413) is a humanized IgG1 MAb targeting the beta 7 integrin subunit. It binds to two integrins, alpha4beta7 and alphaEbeta7. These integrins are required for lymphocyte trafficking and retention, respectively, in the gastrointestinal tract and appear to play a role in inflammatory bowel diseases.

Lebrikizumab is a novel humanized monoclonal antibody designed to specifically block the action of the interleukin-13 cytokine (a signalling protein that serves as a messenger between cells that is increased in some patients with asthma) and so reduce airway inflammation, a key feature of asthma.

Omalizumab (Xolair) is a monoclonal antibody that specifically targets the antibody IgE (immunoglobulin E). Xolair is designed to bind to the circulating IgE antibodies in the blood, decreasing the amount of IgE antibodies available to bind to mast cells.Xolair is being tested in Chronic Idiopathic Urticara (hives) For Xolair full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.xolair.com or call 1-866-4XOLAIR.

Rituxumab (Rituxan) is a therapeutic antibody that targets and selectively depletes CD20-positive B-cells without targeting stem cells or existing plasma cells. It is being studied in autoimmune diseases with significant unmet medical needs. For full prescribing information, please visit http://www.rituxan.com.

A phase III study in enthesopathy (lateral epicondylitis, patellar tendinitis, achilles tendinopathy, and plantar fasciitis) is ongoing to evaluate the reduction of pain by Suvenyl. It is being tested to see its effect on pain and stress occurring where tendon and ligament meet the bone.

Tocilizumab (Actemra/RoACTEMRA) is a humanised monoclonal antibody to the interleukin-6 receptor, inhibiting the activity of interleukin-6 , a protein that plays a major role in the rheumatoid arthritis inflammation process. For Actemra full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.actemra.com or call 1-800-FDA-1088.

Crenezumab (Anti-Abeta, MABT5102A, RG7412) is a humanized monoclonal antibody, which binds to amyloid beta (Abeta). Abeta is the main constituent of amyloid plaque in the brains of patients with Alzheimer's disease and is proposed to be causative in the development of the disease.

Mechanism of Action / Target

Gantenerumab is a fully human monoclonal antibody that binds and neutralises disease-relevant aggregated forms of amyloid-beta: those that accumulate as plaques in the brain and those which interfere with brain-cell functioning.

Tofogliflozin, an oral, small molecule sodium-glucose cotransporter 2 (SGLT2) inhibitor, blocks the activity of SGLT2. SGLT2 is a protein in the kidneys responsible for the reabsorption of filtered glucose to prevent glucose excretion into the urine. Tofogliflozin’s efficacy in increasing renal glucose excretion is currently studied in patients with type 2 diabetes.

Anti-Influenza A (MHAA4549A, RG7745) is a human monoclonal antibody that binds to a highly conserved epitope on the influenza A hemagglutinin stalk region, which is designed to neutralize the influenza A virus across a broad range of different strains.

Mechanism of Action / Target

Lampalizumab (Anti-Factor D Fab, FCFD4514S, RG7417) is a humanized monoclonal antibody fragment targeting complement factor D. It is designed to inhibit complement activation in tissues. Complement Factor D is critical for alternative complement pathway activation which is hypothesized to generate inflammatory responses that contribute to GA development and progression.

Ranibizumab: ranibizumab (Lucentis) is a monoclonal antibody fragment. It is designed to bind to and inhibit VEGF (vascular endothelial growth factor), a protein that is believed to play a critical role in the formation of new blood vessels (angiogenesis) and the hyperpermeability (leakiness) of the vessels. Ranibizumab is being tested for sustained delivery in DME. In DME, damaged blood vessels leak fluid into the central portion of the retina, called the macula, causing it to swell. The macula is the part of the eye responsible for sharp central vision.